| Bioactivity | B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor (Ki of 4.2 nM; IC50=15.1 nM). B022 protects liver from toxin-induced inflammation, oxidative stress, and injury[1][2]. | ||||||||||||
| Target | Ki: 4.2 nM (NF-κB-inducing kinase (NIK)) | ||||||||||||
| Invitro | B022 (0-5 μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner[1].B022 (0-5 μM; 12 hours; Hepa1 cells) treatment for 8 h completely blocks NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5[1]. B022 prevents NIK- or H2O2-induced β cell death and also ameliorates streptozotocin (STZ)-induced β cell death and hyperglycemia[3]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| In Vivo | B022 (30 mg/kg; intravenous injection; twice a day; for 10 days; STOP-NIK male mice) treatment inhibits NIK-triggered liver inflammation and injury in STOP-NIK mice infected with cre adenoviruses[1]. Animal Model: | ||||||||||||
| Name | B022 | ||||||||||||
| CAS | 1202764-53-1 | ||||||||||||
| Formula | C19H16ClN5OS | ||||||||||||
| Molar Mass | 397.88 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ren X, et al. A small-molecule inhibitor of NF-κB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury. FASEB J. 2017 Feb;31(2):711-718. [2]. Li Z, et al. Discovery of a Potent and Selective NF-κB-Inducing Kinase (NIK) Inhibitor That Has Anti-inflammatory Effects in Vitro and in Vivo. J Med Chem. 2020;63(8):4388-4407. [3]. Li X, et al. Activation of NF-κB-Inducing Kinase in Islet β Cells Causes β Cell Failure and Diabetes. Mol Ther. 2020;28(11):2430-2441. |